This invention is concerned with trifluoromethylthio derivatives of cyproheptadine which are potent antipsychotic agents, particularly the levorotatory enantiomer, and platelet aggregation inhibitors useful as antithrombotic agents.
Traditionally, in the dibenzocycloheptene series of compounds, those with a piperidinylidene group in the 5-position have been considered to be without notable antipsychotic action. Recently, however, 3-cyanocyproheptadine, and particularly the levorotatory isomer was found to have antipsychotic activity and the dextrorotatory isomer was found to have anticholinergic activity.
Furthermore, racemic 3-trifluoromethylthiocyproheptadine has been disclosed in British Pat. No. 1,336,335 but only as an intermediate in the synthesis of novel therapeutically useful compounds. There is no disclosed pharmacological activity for the compound itself and no suggestion that the compound exists as enantiomers or that the enantiomers would exhibit different pharmacological activities.
Surprisingly, it has now been found that levorotatory trifluoromethylthio derivatives of cyproheptadine are potent antipsychotic agents, and that both enantiomers thereof are platelet aggregation inhibitors useful as antithrombotic agents.
It is thus an object of the present invention to provide (-)- and (+)-trifluoromethylthiocyproheptadine derivatives as novel compounds with the aforementioned utilities.
It is a further object of this invention to provide novel processes for the preparation of the novel compounds.
Another object of the invention is to provide novel pharmaceutical compositions comprising the novel compounds or mixtures thereof as active ingredient.
Another object of the invention is to provide a novel method of treating psychoses by administration of the levorotatory or racemic compounds or pharmaceutical compositions thereof to a patient.
It is also an object of this invention to provide a novel method of treatment of thrombosis by administration of the novel compounds or mixtures thereof, or pharmaceutical compositions thereof to a patient.